Biochem/physiol Actions
LY2784544 is an orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK2, 19.8 nM/20 μM/JAK1, 48.0 nM/2 μM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 μM) GPR39 agonist activity, but not 11 other GPRs.
Orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor with additional Zn+2-dependent GPR39 agonist activity.
| assay | ≥98% (HPLC) |
| form | powder |
| composition | H2O, 0-4 mol/mol (moles per mole of product) |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| web metadata keyword.default | 3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine for research,JAK2-selective inhibitor LY2784544 for cancer studies,LY2784544 1229236-86-5 CAS number,LY2784544 ATP-competitive kinase inhibitor,LY2784544 JAK2 inhibitor for drug discovery,LY2784544 JAK2 inhibitor,LY2784544 chemical structure and applications,LY2784544 for laboratory use,LY2784544 for oncology research,LY2784544 high purity for pharmacological studies,LY2784544 janus kinase inhibitor for clinical trials,LY2784544 potency and efficacy in JAK2V617F models,LY2784544 procurement for biotech applications |
| storage temp. | 2-8°C |
| SMILES string | Fc1c(ccc(c1)Cl)Cc2[n]3c(nc2C)C(=CC(=N3)Nc5n[nH]c(c5)C)CN4CCOCC4 |
| InChI | 1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30) |
| InChI key | SQSZANZGUXWJEA-UHFFFAOYSA-N |
